产品说明书
Rosiglitazone maleate
 |
同义名 : | BRL 49653C;Rosiglitazone (maleate);Avandaryl;Avandia |
| CAS号 : | 155141-29-0 | |
| 货号 : | A332359 | |
| 分子式 : | C22H23N3O7S | |
| 纯度 : | 98% | |
| 分子量 : | 473.499 | |
| MDL号 : | MFCD03427306 | |
| 存储条件： |
粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(221.75 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Rosiglitazone maleate, a potent and selective activator of PPARγ, exhibits EC50 values of 30 nM and 100 nM for PPARγ1 and PPARγ2, respectively, and a Kd of approximately 40 nM for PPARγ. Rosiglitazone (BRL49653) at concentrations of 0.1, 1, 10 μM, promotes the differentiation of C3H10T1/2 stem cells into adipocytes[1]. Rosiglitazone activates PPARγ with an EC50 of 60 nM[2]. Rosiglitazone (1 μM) activates PPARγ, which binds to the NF-α1 promoter, enhancing gene transcription in neurons. Additionally, Rosiglitazone (1 μM) protects Neuro2A cells and hippocampal neurons against oxidative stress and upregulates BCL-2 expression in an NF-α1-dependent manner[3]. Rosiglitazone effectively blocks TRPM3 channels with IC50 values of 9.5 μM and 4.6 μM against nifedipine- and PregS-evoked activities, respectively, through mechanisms not involving PPARγ. It also inhibits TRPM2 channels at a higher concentration, with an IC50 of approximately 22.5 μM. Additionally, Rosiglitazone acts as a potent activator of TRPC5 channels, with an EC50 of about 30 μM[4]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| HepG2 cells | Function assay | Peroxisome proliferator activated receptor gamma agonistic activity in HepG2 cells, EC50=0.73 μM | 10714503 | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00306696 | Diabetes Mellitus | Phase 4 | Completed | - | - |
| NCT00367055 | Type 2 Diabetes Mellitus | Phase 4 | Completed | - | - |
| NCT00367055 | - | Completed | - | - | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.11mL 0.42mL 0.21mL |
10.56mL 2.11mL 1.06mL |
21.12mL 4.22mL 2.11mL |
| 参考文献 |
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